Day: November 13, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1098340-27-2,Methyl 4-(trifluoromethyl)-1H-indole-2-carboxylate,as a common compound, the synthetic route is as follows.,1098340-27-2

General procedure: Method B: to a solution of N-chlorosuccinimide (1.2 eq.) in DMF (0.3 M) was added sodium iodide (1.2 eq.) in small portion. The resulting brown solution was stirred at room temperature for 1 h before the slow addition at 0 C of the corresponding indole (1.0 eq.) in DMF (0.3 M). The reaction mixture was stirred at room temperature overnight. A saturated aqueous solution of sodium thiosulfate and water were added and the mixture was stirred for 1 h. After filtration, the crude material was washed with cold water and cold petroleum ether to afford after drying under high vacuum the attempted 3-iodoindole which was used in the next step without any further purification. Compounds 24 (method B), 22-35 (method A) were previously described [11], [18] and [19].

The synthetic route of 1098340-27-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Neagoie, Cleopatra; Vedrenne, Emeline; Buron, Frederic; Merour, Jean-Yves; Rosca, Sorin; Bourg, Stephane; Lozach, Olivier; Meijer, Laurent; Baldeyrou, Brigitte; Lansiaux, Amelie; Routier, Sylvain; European Journal of Medicinal Chemistry; vol. 49; (2012); p. 379 – 396;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

487-89-8, Indole-3-carboxaldehyde is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The 1.0 g of indole -3 – formaldehyde is dissolved in 15 ml in tetrahydrofuran, then the 0.5 g of […] add the above-mentioned solution, stirring at room temperature 5 h, then adding 1.5 g benzene sulfonyl chloride, continuing to stir 8 h. Thin-layer chromatographic monitoring. After the reaction, the reaction solution is added to quench the reaction, then ethyl acetate – extraction with water, dried with anhydrous sodium sulfate ethyl acetate, concentrated solution, to obtain 1.7 g solid compound II. Yield 86.5%., 487-89-8

As the paragraph descriping shows that 487-89-8 is playing an increasingly important role.

Reference£º
Patent; Southern Medical University; Chen Jianjun; Li Gang; (11 pag.)CN109776528; (2019); A;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

1075-35-0, 5-Chloro-2-methylindole is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of 2-(3-pyrroline-1-yl) arylaldehydes 1 (0.5mmol, 1.0equiv), indoles 2 (0.55mmol, 1.1equiv) in ethylenechloride (5mL) was added diphenyl phosphite (0.1mmol, 0.1equiv). The mixture was stirred at ambient temperature overnight and the reaction was monitored by TLC. After completed, the reaction was concentrated under reduced pressure and purified by flash chromatography on silica gel (petroleum ether: ethyl acetate=20:1)., 1075-35-0

As the paragraph descriping shows that 1075-35-0 is playing an increasingly important role.

Reference£º
Article; Lei, Xiantao; Xie, Hong-Yan; Chen, Si-Yuan; Teng, Kai-Shun; Wen, Xiaoan; Xu, Qing-Long; Sun, Hongbin; Tetrahedron; vol. 71; 24; (2015); p. 4098 – 4101;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

2380-86-1, 1H-Indol-6-ol is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To amixture of compound 10 (1.17 g, 8.78mmol) and Cs2CO3, (3.43 g, 10.54 mmol) in MeCN (30 mL)was added benzyl bromide (1.79 g, 10.54 mmol) and stirred at room temperature for6 h. After the reaction was completed, to the reaction mixture was added water,diluted and extracted with EtOAc. The combined organic extracts were washedwith water and brine, dried over anhydrous MgSO4, filtered, andconcentrated under reduced pressure. The residue was purified by silica gelcolumn chromatography (n-hexane:EtOAc = 2:1) to afford 1.41 g (6.32 mmol, 72percent) of the title compound 11 as gray solid; Rf= 0.34 (n-hexane : EtOAc = 2:1); 1H NMR (400MHz, CDCl3) delta 7.85 (NH, br s), 7.29-7.51 (6H, m), 6.96 (1H, d, J?= 2.0Hz), 6.81-6.88 (2H, m), 6.44 (1H, s), 5.03 (2H, s); 13C NMR (100MHz, CDCl3) delta 155.5, 137.5, 136.4, 128.6, 127.9, 127.6, 123.3, 122.4,121.3, 110.7, 102.4, 96.0, 70.7; IR (neat, cm-1) 3384,3030, 2859, 1625, 1455, 1091., 2380-86-1

The synthetic route of 2380-86-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Gim, Hyo Jin; Li, Hua; Jeong, Ji Hye; Lee, Su Jeong; Sung, Mi-Kyung; Song, Mi-Young; Park, Byung-Hyun; Oh, Soo Jin; Ryu, Jae-Ha; Jeon, Raok; Bioorganic and Medicinal Chemistry; vol. 23; 13; (2015); p. 3322 – 3336;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

474799-41-2, 6-Nitroindolin-2-one is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,474799-41-2

Triethylamine (3.91 rnL, 28.0 mmol) and Z4 (1.0 g, 5.61 mmol) are added successively to furan-2-carboxylic acid (1.32 g, 11.79 mmol) and TBTU (3.79 g, 11.79 mmol) in anhydrous DMF (5 mL) and the mixture is stirred for 24 h at RT. The reaction mixture is in poured into 1 N HCl: MeOH = 1 : 1, the precipitate is suction filtered and digested with iPrOH. Yield: 1.60 g (78 percent).Alternatively CH2Cl2 may be used as solvent. If no crystalline product is obtained, the reaction mixture is worked up by extraction and the residue is optionally chromatographed.

474799-41-2 6-Nitroindolin-2-one 17960994, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; WO2008/152013; (2008); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

16732-70-0, Ethyl 5-bromo-1H-indole-2-carboxylate is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 5-bromoindole-2-carboxylic acid ethyl ester (3.48 g, 13 mmol), 4-terr-butylphenylboronic acid (4.63 g, 26 mmol), K3PO4 (9.93 g, 45 mmol), Pd(OAc)2 (146 mg, 0.65 mmol), tri-o-tolylphosphine (396 mg, 25 30 1.3 mmol), EtOH (20 ml) and toluene (10 mL) was stirred under argon for 20 min at rt foolowed by heating at 100 0C for 24 h. The mixture was allowed to cool to rt, poured into NaHCO3 (aq, sat) and extracted with EtOAc. The combined extracts were washed with water and brine, dried (Na2SO4), concentrated and purified by chromatography to give the sub-title compound (3.27 g, 78%)., 16732-70-0

The synthetic route of 16732-70-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOLIPOX AB; WO2006/77367; (2006); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.58665-00-2,Methyl 2-(1-methyl-1H-indol-3-yl)acetate,as a common compound, the synthetic route is as follows.

58665-00-2, A solution of 2-(trifluoromethyl) aniline (161 mg, 1 mmol) in 5 ml of dry tetrahydrofuran was added via syringe to a vigorously stirred mixture of (L-METHYL-LH- indol-3-yl) -acetic acid methyl ester (4 mmol) and LDA (4 mmol, freshly prepared from DIISOPROPYLAMINE and n-BuLi) in 20 ml of dry THF AT-78 C under argon. The mixture was allowed to warm to room temperature and stirred for an additional 4 H. The resulting solution was concentrated in vacuo. The residue was partitioned between ETOAC, and concentrated aqueous NH4C1, and the aqueous layer was extracted with EtOAc. Combined organic extracts were dried over NA2S04, concentrated I71 vacuo, and purified by column chromatography (Silica gel, HEXANE/ETOAC = 1 : 3) to afford analytically pure 4-fluoro-3- (1-methyl-1H-indol-3-yl)-1H-quinolin-2-one.

The synthetic route of 58665-00-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; IMCLONE SYSTEMS INCORPORATED; WO2004/89930; (2004); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

23077-44-3, 6-Fluoro-1H-indole-3-carboxylic acid is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of 1H-indole-3-carboxylic acid (3) (161 mg,1.0 mmol, 1 equiv) in DMF (10 mL) or 3-(2-(1H-indol-3-yl)-1Himidazol-5-yl)benzoic acid (4) (303 mg, 1 equiv) at 0 C was addedDIPEA (0.21 mL, 1.2 mmol, 1.2 equiv). The resulting mixture wasstirred at 0 C for 30 min followed by dropwise addition of theappropriate a-bromoketone (1.1 mmol, 1.1 equiv) in DMF. Theresulting mixture was stirred at 0 C for 4 h, and then quenchedwith ice-water. The precipitated solid was filtered, washed withwater and dissolved in EtOAc. The organic phasewaswashed with a1 N HCl aqueous solution, and then a saturated NaHCO3 aqueoussolution, then H2O, dried over MgSO4, and concentrated in vacuo,which was used in the next stage without further purification. Tothis product, AcOH (25 mL) and AcONH4 (924 mg, 12 mmol, 12equiv)was added and the resulting suspensionwas refluxed for 5 h,cooled to room temperature, concentrated in vacuo and dilutedwith crushed ice. The brown solid was filtered, washed thoroughlywith water. The crude cake was dissolved in EtOAc washed with asaturated NaHCO3 aqueous solution and with H2O, dried overMgSO4, and concentrated in vacuo. The crude product was purifiedby flash chromatography on silica gel (DCM/EtOAc, 8/2 to 7/3) togive imidazole derivatives 4a-4b or 10a-10b.

23077-44-3, As the paragraph descriping shows that 23077-44-3 is playing an increasingly important role.

Reference£º
Article; Tarazi, Hamadeh; Odeh, Raed Abu; Al-Qawasmeh, Raed; Yousef, Imad Abu; Voelter, Wolfgang; Al-Tel, Taleb H.; European Journal of Medicinal Chemistry; vol. 125; (2017); p. 1213 – 1224;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1670-83-3,Indole-7-carboxylic acid,as a common compound, the synthetic route is as follows.

Example 7; Preparation of 1H-Indole-7-carboxylic acid (4-tert-butyl-benzyl)-[2-(4-methoxy-phenyl)-ethyl]-amide; To a solution of 48 mg (0.3 mmol) of 1H-indole-7-carboxylic acid and 96 mg of TBTU (0.3 mmol) in 4 ml DMF, were added 0.26 ml (1.5 mmol) of N,N-diisopropylethyl amine. After stirring for 5 min at rt, 89 mg (0.3 mmol) (4-tert-butyl-benzyl)-[2-(4-methoxy-phenyl)-ethyl]-amine in 1 ml DMF was added. After 2.5 h stirring at rt, the reaction mixture was diluted with 50 ml water and extracted with 2¡Á50 ml EtOAc. The combined organic phases were washed with water and brine, dried with magnesium sulfate, filtered and concentrated in vacuo. The yellow solid foam was purified by column chromatography (8 g silica gel; heptane/EtOAc 6:1) to give 107 mg (80%) of a white solid. MS (ISP) 441.4 (M+H)+.

1670-83-3, As the paragraph descriping shows that 1670-83-3 is playing an increasingly important role.

Reference£º
Patent; Conte-Mayweg, Aurelia; Kuehne, Holger; Luebbers, Thomas; Maugeais, Cyrille; Mueller, Werner; Pflieger, Philippe; US2006/30613; (2006); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

883535-89-5,883535-89-5, 2-(2-Methyl-1H-indol-1-yl)ethanamine is a indole-building-block compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A solution of 2-(2-methyl-1H-indol-1-yl)ethanamine (4a) (65 mg, 0.373 mmol) and 4-(piperidin-1-yl)benzoic acid (5) (76 mg, 1 eq.), and dimethylaminopyridine (catalytic, ?5 mg) in dichloromethane (6 mL) was added 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide.hydrochloride (EDCI) (92 mg, 1.3 eq.) at room temperature. The resulting reaction mixture was stirred for 6h. At the conclusion of the reaction (TLC), water (15 mL) was added to quench the reaction. The product was extracted with ethyl acetate (20mL¡Á3). Organics were washed with dilute HCl (10 mL), saturated NaHCO3 solution (10 mL), water (10 mL) and brine solution (10 mL) and dried over Na2SO4 and concentrated. The resulting crude product was subjected to silica gel chromatography eluting with 0-40% ethyl acetate in hexane to furnish 7k (TG7-152) (100mg, 74% yield). 1H NMR (CDCl3): delta 7.52 (d, J=5.6Hz, 1H), 7.49 (d, J=8.8Hz, 2H), 7.30 (d, J=8Hz, 1H), 7.07 (m, 2H), 6.80 (d, J=8.2Hz, 2H), 6.23 (s, 1H), 5.98 (t, J=5.4Hz, 1H), 4.33 (t, J=6Hz, 2H), 3.76 (q, J=6Hz, 2H), 3.25 (t, J=4.8Hz, 4H), 2.37 (s, 3H), 1.6 (m, 6H). LCMS (ESI): >97% purity at lambda 254, MS; m/z, 362 [M+H]+. Anal. Calcd. for C23H27N3O: C, 76.42; H, 7.53; N, 11.62; found; C, 76.48; H, 7.55; N, 11.59.

The synthetic route of 883535-89-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Ganesh, Thota; Jiang, Jianxiong; Dingledine, Ray; European Journal of Medicinal Chemistry; vol. 82; (2014); p. 521 – 535;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles